ボノプラザンフマル酸塩

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

ボノプラザンフマル酸塩 化学特性,用途語,生産方法

• 効能

  消化性潰瘍薬, プロトンポンプ阻害薬

• 商品名

  タケキャブ (武田薬品工業)

• 化学的特性

  Vonoprazan fumarate is white to nearly white crystals or crystalline powder which melts at 194.8°C . It can be dissolved in dimethyl sulfoxide, but has limited solubility in N,N-dimethylacetamide, N,N-dimethylformamide, methanol, and water. It is only slightly soluble in ethanol (99.5%), and has very low solubility in 2-propanol, acetone, 1-octanol, and acetonitrile.

• 利点

  Compared with traditional irreversible proton pump inhibitors (such as omeprazole, esomeprazole, etc.), Vonoprazan fumarate advantages:
  ① The onset of action is good, and the maximum acid-suppressing effect will be achieved on the first day of administration;
  ② Oral administration, not affected by gastric acid damage;
  ③It can improve the phenomenon of acid breakthrough at night.

• 一般的な説明

  Vonoprazan fumarate (TAK-438) is a new oral anti-gastric acid drug jointly launched by Takeda Pharmaceutical and Otsuka Pharmaceutical. It can be used for the treatment of erosive esophagitis, gastric ulcer and duodenal ulcer.

• 作用機序

  Vonoprazan fumarate is a potassium ion (K+) competitive acid blocker (P-CAB), which is a reversible proton pump inhibitor. It can inhibit the combination of K+ and H+-K+-ATPase (proton pump), so that secretion of gastric acid is terminated. Vonoprazan fumarate has a strong and lasting inhibitory effect on gastric acid secretion.

• 合成

  Vonoprazan FuMarate is prepared by the reaction of vonoprazan and (2E)-but-2-enedioic acid. The steps are as follows:
  Step 1: (2E)-but-2-enedioic acid With sodium hydroxide In water at 50 - 60℃.
  Step 2: vonoprazan In water; toluene at 25 - 35℃; Reagent/catalyst.
  Add 730g of water and 73g of fumaric acid to a 2L reaction flask at 5060, stir and disperse, control the temperature between 5060, add 25g of hydrogen hydroxide dropwise to the fumaric acid suspension The solution of sodium and 300 g of water was gradually dissolved in the system during the dropwise addition, and the aqueous solution of compound was obtained and kept for use.Between 25 and 35°C, take half of the toluene solution of compound obtained in the previous step and put it into a 5L reaction flask, and add the aqueous solution of the above compound dropwise to it. During the dropwise addition, the system has a white solid precipitation. After the dropwise addition was completed, keep stirring for 2-4 hours, filter, and dry the filter cake at 50°C to obtain 131.32 g of white solid, the HPLC purity was 99.96%, and the yield was 94%.
  

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881681-01-2, ボノプラザンフマル酸塩 キーワード